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Eluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them

Inactive Publication Date: 2005-02-10
TEVA PHARM USA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, the method is not advantageous where the effectiveness of a drug correlates with peak bloodstream levels of the drug, as in the case of statin drugs.
Water has been implicated in drug stability problems.

Method used

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  • Eluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them
  • Eluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them
  • Eluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them

Examples

Experimental program
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Effect test

example 1

Fluvastatin methyl ester (3.0 g) was dissolved in acetone (30 ml) and NaOH (0.29 g) partially dissolved in acetone (0.75 ml) was added. The mixture was stirred at room temperature overnight. The product was isolated by filtration under nitrogen, washed with acetone (40 ml) and dried at 50° C. in a vacuum oven for 24 h to obtain 2.31 g (76.2%) of fluvastatin sodium crystal Form I.

example 2

Fluvastatin methyl ester (3.01 g) was dissolved in acetonitrile (60 ml) by heating and NaOH (0.28 g) was added. The mixture was stirred at about 60° C. for 1 h, cooled to room temperature, heated again to about 75° C. for 2 h, then cooled to room temperature and stirred overnight. The product was isolated by filtration under nitrogen, washed with acetonitrile (40 ml) and dried at 50° C. in a vacuum oven for 24 h to obtain 1.07 g (34.9%) of fluvastatin sodium crystal Form I.

example 3

Fluvastatin methyl ester (3.01 g) was dissolved in acetonitrile (60 ml) by heating and a solution of NaOH (0.28 g) in water (0.75 ml) was added at about 50° C. The mixture was stirred at about 40° C. for 2 h, cooled to room temperature and stirred for another h. The product was isolated by filtration under nitrogen, washed with acetonitrile (40 ml) and dried at 50° C. in a vacuum oven for 24 h to obtain 2.52 g (82.2%) of fluvastatin sodium crystal Form I.

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Abstract

Provided are polymorphic forms of fluvastatin sodium and processes for their preparation.

Description

FIELD OF THE INVENTION The present invention relates to the antihypercholesterolemia and antilipidemia agent fluvastatin and, more particularly, to the solid state properties of its monosodium salt. BACKGROUND OF THE INVENTION Complications of cardiovascular disease, such as myocardial infarction, stroke, and peripheral vascular disease account for half of the deaths in the United States. A high level of low density lipoprotein (LDL) in the bloodstream has been linked to the formation of coronary lesions which obstruct the flow of blood and can rupture and promote thrombosis. Goodman and Gilman, The Pharmacological Basis of Therapeutics 879 (9th ed. 1996). Reducing plasma LDL levels has been shown to reduce the risk of clinical events in patients with cardiovascular disease and in patients who are free of cardiovascular disease but who have hypercholesterolemia. Scandinavian Simvastatin Survival Study Group, 1994; Lipid Research Clinics Program, 1984a, 1984b. Statin drugs are cur...

Claims

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Application Information

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IPC IPC(8): A61P3/06C07D209/24
CPCC07D209/24C07D209/12A61P3/06A61P43/00A61P9/04A61P9/10A61K31/404C07B2200/13A61K31/405
Inventor LIFSHITZ-LIRON, REVITALKOLTAI, TAMASARONHIME, JUDITHPERLMAN, NURITAVHAR-MAYDAN, SHARON
Owner TEVA PHARM USA INC
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